1. Stem Cell/Wnt TGF-beta/Smad Apoptosis
  2. Organoid TGF-β Receptor Apoptosis
  3. SB-431542

SB-431542 是 TGF-β 受体激酶抑制剂 (TRKI)。SB-431542 对 ALK4、ALK5 和 ALK7 活性有抑制作用, IC50 值分别为 1 μM、0.75 μM 和 2 μM。SB-431542 还能抑制 TGF-β 诱导的转录、基因表达、细胞凋亡和生长抑制。SB-431542 可用于癌症及其信号转导途径的研究。

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SB-431542 Chemical Structure

SB-431542 Chemical Structure

CAS No. : 301836-41-9

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10 mM * 1 mL in DMSO ¥880
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5 mg ¥500
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10 mg ¥800
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50 mg ¥3380
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 161 篇科研文献

WB
RT-PCR

    SB-431542 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2023 Mar 16;161:114537.  [Abstract]

    SB431542 (4.2 mg/kg; i.p.; single daily for 3 days) reduces the expression of α-SMA, collagen-I and p-Smad3 in SiO2-induced fibrosis lungs of mice.

    SB-431542 purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot analyses show the repression of SMC specific markers in the sh-GPM6B TGF-β1 group are abolished by Alantolactone in the sh-GPM6B and the enrichment of SMC specific markers in the GPM6B-sgRNA cells is cancelled by treatment with SB431542.

    SB-431542 purchased from MCE. Usage Cited in: Stem Cells. 2019 Feb;37(2):190-201.  [Abstract]

    Western blot images show Smad2/3 phosphorylation is lower than baseline in the sh-GPM6B cells and higher than baseline in the GPM6B-sgRNA cells. The phosphorylation of Smad2/3 in the sh-GPM6B TGF-β1 group is elevated by Alantolactone and the phosphorylation is reduced by treatment with SB431542.

    SB-431542 purchased from MCE. Usage Cited in: Mol Med Rep. 2019 Mar;19(3):2107-2114.  [Abstract]

    Effects of the TGF‑β1 inhibitor SB (20 μM) on mechanical force‑induced COL‑1 and MMP‑1 mRNA expression.

    SB-431542 purchased from MCE. Usage Cited in: Phytother Res. 2019 Jan;33(1):214-223.  [Abstract]

    Western analysis of FN and α-SMA in cardiac fibroblasts or NIH3T3 with treatments of (+)‐isobicyclogermacrenal, spathulenol, oxymatrine (OMT), and SB431542 at indicated concentrations.

    SB-431542 purchased from MCE. Usage Cited in: Mol Oncol. 2018 Mar;12(3):305-321.  [Abstract]

    Western blot analysis of EGFR, total and phosphorylated Smad3, total and phosphorylated ERK protein expression in cell lysates from two breast cancer cells pretreated with SB431542 and then stimulated with TGF-β for the indicated times.

    SB-431542 purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 May 23;19(6). pii: E1556.  [Abstract]

    E-cadherin, N-cadherin, Snail, and MMP-2 expression in HCC cells is examined by Western blot analysis. GAPDH is used as a loading control.

    SB-431542 purchased from MCE. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4354-4365.  [Abstract]

    p-FOXO3a (Thr32), p-FOXO3a (Ser253), FOXO3a, p-Akt and Akt expression via western blot following treatment with PBS, ASV, TGF-b1, TGF-b1+ASV, TGF-b1+SB431542 or TGF-b1+LY294002.

    SB-431542 purchased from MCE. Usage Cited in: Immunol Lett. 2019 Feb;206:33-40.  [Abstract]

    Monocytes were cultured with 20 ng/mL M-CSF with or without 10 ng/mL TGF-β1 for 2 days, with SB431542 (1 or 50 μM) or SIS3 (2.5 μM) having been added 30 min beforehand. Whole-cell lysates were subjected to SDS-PAGE and immunoblotted.

    SB-431542 purchased from MCE. Usage Cited in: Mol Cell Biochem. 2018 Feb;439(1-2):117-129.  [Abstract]

    Protein expression levels of E-cadherin N-cadherin, p-ERK, ERK, TGF-β1, p-Smad2, and p-Smad3 in each group are analyzed by western blotting.

    SB-431542 purchased from MCE. Usage Cited in: Brain Res Bull. 2018 May;139:38-47.  [Abstract]

    pSmad2/3 protein levels are down-regulated by the ALK5 inhibitor SB431542 (rGDF11 group vs. rGDF11+SB group, p=0.000).

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Mar;15(3):2801-2806.  [Abstract]

    A549 cells are co cultured with 10.0 mM SB431542 for 48 h, the expression of TGF β1, Smad2 and caspase 3 are tested by western blot analysis and then analyzed.

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Jun;15(6):9681-9686.  [Abstract]

    A549 cells are treated with 1.0% CSE with or without 10.0 mM SB431542 for 48 h, the levels of TGF β1, p Smad2, and MMP3 is assayed by western blot analysis.

    SB-431542 purchased from MCE. Usage Cited in: Int J Mol Sci. 2017 Apr 18;18(4). pii: E853.  [Abstract]

    The protein level of Six2 and Ki67 after the treatment of phosphorylation Smad3 ( p-Smad3) inhibitor SB431542 (10 µM) for 48 h.

    SB-431542 purchased from MCE. Usage Cited in: Oncol Lett. 2017 Jul;14(1):541-546.  [Abstract]

    To investigate the effect of SB431542 on the accumulation of TGFβ1 and MMP3 in MM cells, RPMI 8226 cells are treated with 10, 100 and 1,000 nmol/mL SB431542 for 48 h. Western blotting is performed. The results demonstrate that SB431542 significantly decreases the accumulation of TGFβ1 and MMP3 at 100 and 1,000 nmol/mL when compared with the control. Smad2, as a signaling molecule, can be initially activated by TGFβ1. Therefore, the effect of SB431542 on the expression of Smad2 and p-Smad2 in RPM

    SB-431542 purchased from MCE. Usage Cited in: Chin J Immun. 2016 (5): 615-619.

    10-1000 nM of SB431542 are co-cultured with RLE-6TN cells for 48 h. Expressions of p-Smad2 and Smad are detected by Western blot.

    SB-431542 purchased from MCE. Usage Cited in: Int Immunopharmacol. 2015 Sep;28(1):707-14.  [Abstract]

    SB431542 is used to block the TGF-β1/Smad2 pathway and the expression of PLTP, p-Smad2 and cleaved caspase-3 is analyzed. (A) RLE-6TN cells are treated with 5–500 nM SB431542 for 72 h. Expression of PLTP and p-Smad2 is analyzed by Western blot. (B) CSE-treated rat lung epithelial cells are treated with 500 nM SB431542 to block the TGF-β1/Smad2 pathway.

    查看 TGF-β Receptor 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways[1][2][3].

    IC50 & Target[1]

    ALK4

    1 μM (IC50)

    ALK5

    0.75 μM (IC50)

    ALK7

    2 μM (IC50)

    体外研究
    (In Vitro)

    SB-431542 可抑制 ALK4、ALK5 和 ALK7 的活性,IC50 值分别为 1 μM、0.75 μM 和 2 μM[1]
    SB-431542 (0- 10 μM;24 小时) 抑制 ALK5 以及激活素 I 型受体 ALK4 和淋巴结 I 型受体 ALK7,它们在激酶结构域中与 ALK5 高度相关[1]
    SB-431542 (0.1、0.5、1、5 或 10 μM;30 分钟) 有效抑制由 TGF-β 和激活素而非 BMP4 诱导的 Smad 磷酸化[1]
    SB-431542 (0-10 μM) 抑制 TGF-β 诱导的转录、基因表达、细胞凋亡和生长抑制[2]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    Cell Line: NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells
    Concentration: 10 μM; 0.1, 0.5, 1, 5, or 10 μM
    Incubation Time: 24 h; 30 min
    Result: Inhibited efficiently phosphorylated Smad2.
    Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1.

    Apoptosis Analysis[2]

    Cell Line: A549 and HT29 cells
    Concentration: 10 μM
    Incubation Time: 24 h
    Result: Inhibited TGF-induced growth suppression and apoptosis.

    Cell Invasion Assay[2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 21 h
    Result: Blocked TGF- induced tumor cell invasion.

    Cell Migration Assay [2]

    Cell Line: A549 cells
    Concentration: 2, 10 μM
    Incubation Time: 5 h , 30 h
    Result: Blocked TGF- induced tumor cell migration.
    体内研究
    (In Vivo)

    SB-431542 (结膜下;0.5 和 2 mM;第 1、2、3 和 7 天) 抑制新西兰兔青光眼滤过手术后的疤痕形成[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3]
    Dosage: 0.5 and 2 mM
    Administration: Subconjunctival injection, on days 1, 2, 3, and 7
    Result: Showed wound healing and less severe scar formation.
    分子量

    384.39

    Formula

    C22H16N4O3

    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (260.15 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 11.17 mg/mL (29.06 mM; 超声加热助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6015 mL 13.0076 mL 26.0152 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (5.41 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.89%

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.6015 mL 13.0076 mL 26.0152 mL 65.0381 mL
    5 mM 0.5203 mL 2.6015 mL 5.2030 mL 13.0076 mL
    10 mM 0.2602 mL 1.3008 mL 2.6015 mL 6.5038 mL
    15 mM 0.1734 mL 0.8672 mL 1.7343 mL 4.3359 mL
    20 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2519 mL
    25 mM 0.1041 mL 0.5203 mL 1.0406 mL 2.6015 mL
    DMSO 30 mM 0.0867 mL 0.4336 mL 0.8672 mL 2.1679 mL
    40 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
    50 mM 0.0520 mL 0.2602 mL 0.5203 mL 1.3008 mL
    60 mM 0.0434 mL 0.2168 mL 0.4336 mL 1.0840 mL
    80 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8130 mL
    100 mM 0.0260 mL 0.1301 mL 0.2602 mL 0.6504 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    SB-431542
    目录号:
    HY-10431
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